产品
编 号:F043093
分子式:C10H12ClNO2
分子量:213.66
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500mg
320
In-stock
1g
432
In-stock
5g
1622
In-stock
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生物活性:
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.

体内研究:
Baclofen (ip;10 μg/g;每天两次,连续 3 天) 改善 YAC128 HD 转基因小鼠的运动缺陷。Animal Model:Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age
Dosage:10 μg/g
Administration:IP; twice daily at 9:00 a.m. and 5:00 p.m., for 3 consecutive days; then single dose on the fourth day at 9:00 a.m
Result:Ameliorated motor deficits in YAC128 HD transgenic mice. Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.

体外研究:
Baclofen (1,10 μM;24 h) 导致乳酸脱氢酶 (LDH) 活性显著降低,表明表达野生型或突变亨廷顿蛋白的纹状体细胞 (HD19 或 HD43) 的细胞活力增加。Baclofen 显著增加 HD43 细胞中的胰凝乳蛋白酶样蛋白酶体活性和细胞活力。
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